[(2S,3S,5S,8R,9S,10S,13S,14S,16S,17R)-17-acetyloxy-10,13-dimethyl-2,16-bis(1-methylpiperidin-1-ium-1-yl)-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl] acetate;dihydrobromide

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 英文名称: [(2S,3S,5S,8R,9S,10S,13S,14S,16S,17R)-17-acetyloxy-10,13-dimethyl-2,16-bis(1-methylpiperidin-1-ium-1-yl)-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl] acetate;dihydrobromide
• 化学式: C35H62Br2N2O4+2
• mdl: MFCD00079223
• 分子量: 734.7
• InChiKey: NPIJXCQZLFKBMV-YTGGZNJNSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3.27
• 重原子数：
  43
• 可旋转键数：
  6
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.942
• 拓扑面积：
  52.6
• 氢给体数：
  2
• 氢受体数：
  4

ADMET

代谢

在猫身上，静脉注射潘库龙溴酸8小时后，尿液中未改变的潘库龙溴酸占剂量的58%，3-羟基衍生物占14.5%，17-羟基衍生物占7%，3,17-二羟基衍生物占4.5%。

IN CATS, 8 HR AFTER IV INJECTION OF PANCURONIUM BROMIDE, UNCHANGED PANCURONIUM BROMIDE IN URINE, BILE, & LIVER ACCOUNTED FOR 58% OF DOSE, 3-HYDROXY-DERIV FOR 14.5%, 17-HYDROXY-DERIV FOR 7% & 3,17-DIHYDROXY-DERIV FOR 4.5%.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

从临床角度来看，这些药物最重要的药理相互作用是与某些全身麻醉药、某些抗生素以及抗胆碱酯酶化合物。/神经肌肉阻滞剂/

FROM CLINICAL VIEWPOINT, MOST IMPORTANT PHARMACOLOGICAL INTERACTIONS OF THESE DRUGS ARE WITH CERTAIN GENERAL ANESTHETICS, CERTAIN ANTIBIOTICS, AND ANTI-CHOLINESTERASE COMPOUNDS. /NEUROMUSCULAR BLOCKING AGENTS/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

二乙醚以及先前的琥珀酰胆碱会增强并延长潘库隆的作用。

...DIETHYL ETHERS, AS WELL AS PRIOR SUCCINYLCHOLINE, INTENSIFY & PROLONG ACTION /OF PANCURONIUM/.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

乙醚对突触后膜有稳定作用，因此与竞争性阻断剂协同作用。... 氟烷、环丙烷、氟氧乙烷、甲氧氟烷和恩氟烷也与竞争性阻断剂协同作用，但作用较小。/神经肌肉竞争性阻断剂/

ETHER EXERTS STABILIZING EFFECT ON POSTJUNCTIONAL MEMBRANE & THEREFORE, ACTS SYNERGISTICALLY WITH COMPETITIVE BLOCKING AGENTS. ... HALOTHANE, CYCLOPROPANE, FLUROXENE, METHOXYFLURANE, & ENFLURANE LIKEWISE ACT SYNERGISTICALLY WITH COMPETITIVE BLOCKING AGENTS, BUT TO LESSER EXTENT. /NEUROMUSCULAR COMPETITIVE BLOCKING AGENTS/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

氨基糖苷类抗生素通过抑制乙酰胆碱从前神经节末梢释放（通过与Ca(2+)竞争）以及通过稳定突触后膜来产生神经肌肉阻滞。这种阻滞可以通过钙盐来拮抗，但只能通过抗胆碱酯酶药物不稳定地拮抗。四环素类抗生素也可以产生神经肌肉阻滞，可能是通过螯合钙离子。其他具有神经肌肉阻滞作用的抗生素还包括多粘菌素B、粘菌素、克林霉素和林可霉素。/神经肌肉阻滞剂/

AMINOGLYCOSIDE ANTIBIOTICS PRODUCE NEUROMUSCULAR BLOCKADE BY INHIBITING ACETYLCHOLINE RELEASE FROM THE PREGANGLIONIC TERMINAL (THROUGH COMPETITION WITH CA(2+)) AND ... BY STABILIZING THE POSTJUNCTIONAL MEMBRANE. THE BLOCKADE IS ANTAGONIZED BY CALCIUM SALTS, BUT ONLY INCONSISTENTLY BY ANTICHOLINESTERASE AGENTS. THE TETRACYCLINE ANTIBIOTICS ALSO CAN PRODUCE NEUROMUSCULAR BLOCK, POSSIBLY BY CHELATION OF CALCIUM IONS. ADDITIONAL ANTIBIOTICS THAT HAVE NEUROMUSCULAR BLOCKING ACTION ... INCLUDE POLYMYXIN B, COLISTIN, CLINDAMYCIN, & LINCOMYCIN. /NEUROMUSCULAR BLOCKING AGENTS/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 非人类毒性摘录

动物因...竞争性阻断剂中毒首先表现出肌无力，最终肌肉变得...弛缓且对运动神经支配无反应。...隔肌和肋间肌最终麻痹，呼吸随之停止。死亡是由外周呼吸麻痹导致的低氧血症引起的。临终时可能出现窒息性惊厥.../神经肌肉阻断剂/

ANIMALS POISONED BY ... COMPETITIVE BLOCKING AGENTS FIRST EXHIBIT MOTOR WEAKNESS, & ULTIMATELY MUSCLES BECOME ... FLACCID & INEXCITABLE THROUGH THEIR MOTOR INNERVATION. ... INTERCOSTAL MUSCLES & FINALLY DIAPHRAGM ARE PARALYZED, & RESP THEN CEASES. DEATH IS CAUSED BY HYPOXIA SECONDARY TO PERIPHERAL RESP PARALYSIS. TERMINAL ASPHYXIAL CONVULSIONS MAY APPEAR ... /NEUROMUSCULAR BLOCKING AGENTS/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

肝脏和肾脏都参与降解和排泄...潘库溴铵...

BOTH LIVER & KIDNEYS ARE INVOLVED IN DEGRADATION & EXCRETION OF ... PANCURONIUM ...

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

静脉注射后，效果在成年人不到3分钟内达到最大，在儿童90秒内达到最大。血浆半衰期可能略少于2小时。泮库溴铵大部分以原形通过尿液排出。

AFTER IV INJECTION, EFFECTS...BECOME MAXIMAL IN LESS THAN 3 MIN IN ADULTS & 90 SEC IN CHILDREN. ... PLASMA HALF-LIFE IS PROBABLY SLIGHTLY LESS THAN 2 HR. PANCURONIUM IS MOSTLY EXCRETED UNCHANGED INTO URINE.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

胎盘传递...潘库溴铵...在给母亲给药后迅速发生，但是胎儿：母体药物浓度比非常低。

PLACENTAL TRANSFER OF...PANCURONIUM BROMIDE...OCCURS RAPIDLY AFTER ADMIN TO MOTHERS, BUT FETAL:MATERNAL DRUG CONCN RATIO ARE VERY LOW.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

在七名接受静脉注射的患者中，潘库溴铵的血浆水平遵循两室动力学，β相半衰期在90至162分钟之间变化。中央室的平均体积为100毫升/千克，而总体分布体积为261毫克/千克。在慢性肾衰竭患者中，血浆清除率显著降低，而总体和中央室的体积显著增加。

PLASMA LEVELS OF PANCURONIUM OBEYED TWO-COMPARTMENT KINETICS IN SEVEN PATIENTS ON IV INJECTION & THE BETA-PHASE HALF-TIME VARIED BETWEEN 90 AND 162 MIN. THE MEAN VOLUME OF THE CENTRAL COMPARTMENT WAS 100 ML/KG, WHILE THE OVERALL DISTRIBUTION VOLUME WAS 261 MG/KG. IN PATIENTS WITH CHRONIC RENAL FAILURE, THE PLASMA CLEARANCE...WAS SIGNIFICANTLY REDUCED, WHILE VOLUMES OF BOTH THE OVERALL & CENTRAL COMPARTMENTS WERE SIGNIFICANTLY INCREASED.

来源:Hazardous Substances Data Bank (HSDB)